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食物对呋喃妥因生物利用度的影响。

The influence of food on nitrofurantoin bioavailability.

作者信息

Rosenberg H A, Bates T R

出版信息

Clin Pharmacol Ther. 1976 Aug;20(2):227-32. doi: 10.1002/cpt1976202227.

Abstract

The effect of food on the absorption of five commercial dosage forms of nitrofurantoin varying widely in drug release and dissolution characteristics was assessed in man after oral administration. Four healthy fasting and nonfasting male subjects received, in a crossover fashion, a single 100-mg dose of microcrystalline nitrofurantoin as an aqueous suspension, three different compressed tablets, and a single 100-mg dose of macrocrystalline nitrofurantoin in a capsule. Both the absorption and the duration of therapeutic urinary concentrations of nitrofurantoin were significantly increased after administration of the five products to nonfasting subjects. The enhancement in the bioavailability of the drug in the presence of food ranged from 20% to 400%, with the greatest absorption-enhancing effect occurring with those dosage forms exhibiting the poorest dissolution characteristics. It is concluded that single-dose comparative bioavailability studies of drug products normally administered with food should be performed in both nonfasting and fasting subjects.

摘要

口服给药后,在人体中评估了食物对五种药物释放和溶解特性差异很大的呋喃妥因市售剂型吸收的影响。四名健康的禁食和非禁食男性受试者以交叉方式接受了单剂量100mg的微晶呋喃妥因水混悬液、三种不同的压制片,以及单剂量100mg的胶囊装大晶型呋喃妥因。向非禁食受试者给药这五种产品后,呋喃妥因的吸收和治疗性尿药浓度持续时间均显著增加。食物存在时药物生物利用度的提高幅度为20%至400%,溶解特性最差的剂型吸收增强作用最大。结论是,通常与食物一起服用的药品的单剂量比较生物利用度研究应在非禁食和禁食受试者中都进行。

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